OINTMENTS, CREAMS, PASTES, GELS, Poulice and PLaster PDF/PPT

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Description

OINTMENTS, CREAMS, PASTES, GELS,
Poulice and PLaster

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 Definition: Semi solid pharmaceutical system comprise a body of
product ,which when applied to skin or accessible mucous
membranes tends to alleviate or treat a pathological condition or
other protection against harmful environment.

Ointm Paste
ents s

Cream
s

Gels/ Poultices

Jelly
Plaster

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Physical properties
Physiological

a) Smooth texture properties
b) Elegant in

appearence a) Non irritating
c) Non dehydrating b) Do not alter
d) Non gritty membrane function
e) Non greasy and non c) Miscible with skin

staining secretion
f) Non hygroscopic

Application properties
a. Easy applicable with efficient drug release
b. High aqueous washibility

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They contain one or more active ingredients dissolved or
uniformly dispersed in a suitable base and any suitable
excipients such as emulsifiers, viscosity increasing
agents, anti microbial agents, antioxidents, or
stabilizing agents.

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of semi-solid dosage
form:

• It is used externally
• Probability of side effect can be reduce
• Local action
• First pass gut and hepatic metabolism is avoided.
• Patient compliance is increased, the drug termination is problematic cases

is facilitated as compared with other routes of drug administration.

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of semi-solid
dosage form:

• There is no dosage accuracy in this type of dosage form
• The base which is used in the semi-solid dosage form can be easily

oxidized.
• If we go out after using semi-solid dosage form problems can occur.

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Ointment Creams Pastes

Gels Poultices Plaster

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Ointments are homogenous, translucent, viscous, semi
solid preparation intended for external application to
skin or mucous membranes. Ointment may be
medicated or not..

❖Applied to mucous membrane or skin

❖Uses

Emollient
Application for active ingredients to the skin
Occlusive

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(CONT.)

Ointment Bases are classified based on their
composition and physical Characteristics.

are classified based on their water solubility

•Oleaginous Bases • Hydrophobic ointment

•Absorption Bases • Hydophilic ointment
• Water-emulsifying ointment

•Water-Removable Bases
•Water-Soluble Bases

are classified based on their therapeutic
activity and penetration to skin
• Epidermic ointment
• Endodermic ointment
• Diadermic ointment

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CLASSIFICATION OF BASES

BASES

WATER EMULSION ABSORPTION OLEAGINOUS
SOLUBLE BASE BASE BASE BASE

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I. OLEAGINOUS BASES
These bases consists of oils and fats (hydrophobic). The most
important are the Hydrocarbons i.e. petrolatum, paraffins and
mineral oils.
The combination of these materials can produce a product of
desired melting point and viscosity.
They ae highly compatible, occlusive and good emollients

(a) Petrolatum (Soft paraffin)
This is a purified mixture of semi-solid hydrocarbons obtained from
petroleum or heavy lubricating oil.
Yellow soft paraffin (Petrolatum; Petroleum jelly)
This a purified mixture of semisolid hydrocarbons obtained from
petroleum.
It may contain suitable stabilizers like, antioxidants e.g. a-tocopherol
(Vitamin E), butylated hydroxy toluene (BHT) etc. Melting range : 38 to
560C.
White soft paraffin (White petroleum jelly, White petrolatum)
This a purified mixture of semisolid hydrocarbons obtained from
petroleum, and wholly or partially decolorized by percolating the yellow
soft paraffin through freshly burned bone black or adsorptive clays.
Melting range : 38 to 560C.

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(b) Hard paraffin (Paraffin)
This is a mixture of solid hydrocarbons obtained from petroleum.
It is colorless or white, odorless, translucent, wax-like substance. It
solidifies between 50 and 570C and is used to stiffen ointment bases.

(c) Liquid paraffin (Liquid petrolatum,; White
mineral oil)
It is a mixture of liquid , hydrocarbons obtained from petroleum. It is
transparent, colourless, odourless, viscous liquid.
On long storage it may oxidize to produce peroxides and therefore, it may
contain tocopherol as antioxidants.
It is used along with hard paraffin and soft paraffin to get a desired
consistency of the ointment. Tubes for eye, rectal and nasal ointments
have nozzles with narrow orifices through which it is difficult to expel
very viscous ointments without the risk of bursting the tube. To facilitate
the extrusion upto 25% of the base may be replaced by liquid paraffins.

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Advantages of hydrocarbons bases:
(i) They are not absorbed by the skin. They remain on the surface as an
occlusive layer that restricts the loss of moisture hence, keeps the skin soft.
(ii) They are sticky hence ensures prolonged contact between skin and
medicament.
(iii) They are almost inert. They consist largely of saturated hydrocarbons,
therefore, very few incompatibilities and little tendency of rancidity are
there.
(iv) They can withstand heat sterilization, hence, sterile ophthalmic
ointments can be prepared with it.
(v) They are readily available and cheap.

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Disadvantages of hydrocarbon bases;
(i) It may lead to water logging followed by maceration of the skin if
applied for a prolonged period.
(ii) It retains body heat, which may produce an uncomfortable feeling of
warmth.
(iii) They are immiscible with water; as a result rubbing onto the surface
and removal after treatment both are difficult.
(iv) they are sticky, hence makes application unpleasant and leads to
contamination of clothes.
(v) Water absorption capacity is very low, hence, these bases are poor in
absorbing exudate from moist lesions.

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II. ABSORPTION BASE
• The term absorption base is used to denote the water absorbing or

emulsifying property of these bases and not to describe their action on the
skin.

• These bases (some times called emulsifiable ointment bases) are generally
anhydrous water insoluble and water unwashable.

• Preparations of this type do not contain water as a component of their
basic formula but if water is incorporated a W/O emulsion results.

• Wool Fat (anhydrous lanolin)
• It is the purified anhydrous fat like substance obtained from the wool of

sheep.

·

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It is practically insoluble in water but can absorb water upto 50% of
its own weight. Therefore it is used in ointments the proportion of water
or aqueous liquids to be incorporated in hydrocarbon base is too large.
· Due to its sticky nature it is not used alone but is used along with
other bases in the preparation of a number of ointments.
e.g. Simple ointment B.P. contains 5% and the B.P. eye ointment base
contains 10% woolfat.

Hydrous Wool Fat (Lanolin)
· It is a mixture of 70 % w/w wool fat and 30 % w/w purified
water. It is a w/o emulsion. Aqueous liquids can be emulsified with it.
· It is used alone as an emollient.
· Example:- Hydrous Wool Fat Ointment B.P.C

Beeswax
It is purified wax, obtained from honey comb of bees.
It contains small amount of cholesterol. It is of two types: (a) yellow
beeswax and (b) white beeswax.

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ADVANTAGES OF ABSORPTION BASES:
(i) They are less occlusive nevertheless, are good emollient.
(ii) They assist oil soluble medicaments to penetrate the skin.
(iii)They are easier to spread.
(iv) They are compatible with majority of the medicaments.
(v) They are relatively heat stable.
(vi) The base may be used in their anhydrous form or in emulsified form.
(vii)They can absorb a large quantity of water or aqueous substances.

DISADVANTAGES:

• Inspite of their hydrophilic nature, absorption bases are difficult to wash.

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III. WATER REMOVABLE BASE

A-WATER MISCIBLE BASES EMULSION

BASE)
1-They are miscible with an excess of water.
2-Ointments made from water-miscible bases are easily removed after use.
3-O/w emulsion
4- can be diluted with water
5- can be used to absorbed exudate (discharge) from skin lesion.
There are three official anhydrous water-miscible ointment bases:-
Example:-
Emulsifying ointment B.P. – contains anionic emulsifier.
Cetrimide emulsifying ointment B.P. – contains cationic emulsifier
Cetomacrogol emulsifying ointment B.P. – contains non-ionic emulsifier

W/O EMULSION BASE O/W EMULSION BASE

Hydrous Hydrous

Will absorb water Will absorb water

Insoluble in water Insoluble in water

Not washable washable

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e.g. Hydrophilic ointment
sodium lauryl sulfate 1% emulsifying agent
steryl alcohol 25% emulsifying ointment
while petrolatum25% oleaginous base
PEG 12% aqueous phase
water 37% aqueous phase

ADVANTAGES OF WATER MISCIBLE BASES:
(i) Readily miscible with the exudates from lesions.
(ii) Reduced interference with normal skin function.
(iii) Good contact with the skin, because of their surfactant content.
(iv) High cosmetic acceptability, hence there is less likelihood of the
patients discontinuing treatment.
(v) Easy removal from the hair.

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B. WATER SOLUBLE BASES
• Water soluble bases contain only the water soluble ingredients and not the

fats or other greasy substances, hence, they are known as grease-less
bases.

• Water soluble bases consists of water soluble ingredients such as
polyethylene glycol polymers (PEG) which are popularly known as
“carbowaxes” and commercially known as “macrogols”.
Unlike water miscible ointment contain no olegenous baase
Like water miscible ointment are washable

Water soluble, water washable non greasable
• The PEGs are mixtures of polycondensation products of ethylene and

water and they are described by numbers representing their average
molecular weights. Like the paraffin hydrocarbons they vary in consistency
from viscous liquids to waxy solids.

• Example:-
Macrogols 200, 300, 400 – viscous liquids
Macrogols 1500 – greasy semi-solids
Macrogols 1540, 3000, 4000, 6000 – waxy solids.

Different PEGs are mixed to get an ointment of desired consistency.

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ADVANTAGES OF PEGS AS OINTMENT BASE:
(a) They are water soluble; hence, very easily can be removed from the
skin and readily miscible with tissue exudates.
(b) Helps in good absorption by the skin.
(c) Good solvent properties. Some water-soluble dermatological drugs,

such as salicylic acid, sulfonamides, sulfur etc. are soluble in this bases.
(d) Non-greasy.
(e) They do not hydrolyze, rancidify or support microbial growth.
(f) Compatibility with many dermatological medicaments.

DISADVANTAGES:
(a) Limited uptake of water. Macrogols dissolve when the proportion of
water

reaches about 5%.
(b) Reduction in activity of certain antibacterial agents, e.g. phenols,

hydroxybenzoates and quaternary compounds.
(c) Solvent action on polyethylene and bakelite containers and closures.

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EXAMPLES OF BASES

Hydrocarbons (mineral oils, petrolatums, paraffins, waxes) Oleaginous
Animal fats/vegetable oils (castor oil, cottonseed oil, olive oil) Bases
Synthetic esters (glyceryl monostearate, butyl stearate,

isopropyl lanolate, stearyl alcohol)

Hydrophilic petrolatum Absorption

Aquaphor Bases

Aquabase

Water-in-oil:

Cold Cream (Petrolatum-Rose Water Ointment) Emulsion
Lanolin Bases
Oil-in-water:

Hydrophilic Ointment

Velvachol

Polyethylene Glycol Ointment Water
Biozyme Ointment, Desenex Ointment, Whitfields Ointment Soluble
Veegum 10% Dermatological base Bases
Veegum 5% Thixotropic lotion

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Ointment Bases are classified based on their
composition and physical Characteristics.

•Oleaginous Bases
•Absorption Bases
•Water-Removable Bases
•Water-Soluble Bases

are classified based on their water solubility
• Hydrophobic ointment
• Hydophilic ointment
• Water-emulsifying ointment

are classified based on their therapeutic
activity and penetration to skin
• Epidermic ointment
• Endodermic ointment
• Diadermic ointment

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Ointment further classified based on their water solubility

Hydrophobic ointments: oleaginous base (hydrocarbon)
Hydrophobic (lipophilic) ointments are usually anhydrous and can absorb
only small amounts of water. Typical bases used for their formulation are
water-insoluble hydrocarbons such as hard, soft and liquid paraffin,
vegetable oil, animal fats, waxes, synthetic glycerides and
polyalkylsiloxanes.

Water-emulsifying ointments: w/o emulsion – water absorption base
o/w emulsion- water miscible base

Water-emulsifying ointments can absorb large amounts of water. They
typically consist of a hydrophobic fatty base in which a w/o agent, such as
wool fat, wool alcohols, sorbitan esters, mono glycerides, or fatty alcohols
can be incorporated to render them hydrophilic. They may also be w/o
emulsions that allow additional quantities of aqueous solutions to be
incorporated. Such ointments are used especially when formulating
aqueous liquids or solutions.

Hydrophilic ointments: water soluble base (PEG-macrogol)
Hydrophilic ointment bases are miscible with water. The bases are usually
mixture of liquid and solid polyethylene glycols (macrogols)

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Classification of ointments According to their therapeutic properties
based on penetration of skin.

(a) Epidermic, (b) Endodermic, (c) Diadermic

(a) Epidermic ointments
These ointments are intended to produce their action on the surface
of the skin and produce local effect.
They are not absorbed.
They acts as protectives, antiseptics and parasiticides.

(b) Endodermic ointments
These ointments are intended to release the medicaments that
penetrate into the skin. They are partially absorbed and acts as
emollients, stimulants and local irritants.

(c) Diadermic ointments
These ointments are intended to release the medicaments that pass
through the skin and produce systemic effects.

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Oleaginous Absorption Oil/Water Water-miscible
Ointment Oint. Bases Emulsion Ointment Bases
Bases Water- Oint.Bases Water soluble

absorption Water-misicble

Comp oleaginous oleaginous oleaginous Polyethylene
osition compounds base + w/o base + water (> Glycols (PEGs)

surfactant 45% w/w) + o/w
surfactant (HLB

>9)

Water anhydrous anhydrous hydrous anhydrous,
Conte hydrous
nt

Affinity hydrophobic hydrophilic hydrophilic hydrophilic
for
Water

Sprea difficult difficult easy moderate to easy
dability

Washa nonwashable nonwashable washable washable
bility

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Stability oils poor; oils poor; unstable, stable
hydrocarbo hydrocarbo especially
ns better ns better alkali soaps

and natural
colloids;

nonionics
better

Drug solids or solids, oils, solid and solid and aqueous
Incorporatio oils (oil and aqueous solutions
n Potential solubles aqueous solutions

only) solutions (small
(small amounts)

amounts)
Drug poor poor, but > fair to good good
Release oleaginous
Potential*
Occlusivene yes yes no no
ss

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Uses protectants, protectants, emollients, drug vehicles
emollients emollients vehicles for

(+/-), (+/-), solid, liquid,
vehicles for vehicles for or non-
hydrolyzabl aqueous hydrolyzabl

e drugs solutions, e drugs
solids, and

non-
hydrolyzabl

e drugs
Examples White Hydrophilic Hydrophilic PEG Ointment,

Petrolatum, Petrolatum, Ointment, Polybase™
White Anhydrous Dermabase

Ointment Lanolin, ™,
Aquabase Velvachol®,

™, Unibase®
Aquaphor®,
Polysorb®

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Selection of the Appropriate Base

The selection of the base of an ointment

depends on many factors:

Patient Factors

The condition of the patient’s skin, e.g. oozing or dry

The rule in dermatology that

if a patient’s skin is dry-wet it, If it is wet-dry it

if a patient’s skin is dry, occlusive ointment base that retain

moisture is preferable

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Physicochemical Factors

1 The desired release rate of the drug from the ointment base

2 The desired enhancement of the percutaneous absorption

of the drug

3 The desired occlusion of moisture from the skin by the base

4 The stability of the drug in the ointment base, for a drug that

hydrolyzes rapidly as antibiotics, a hydrocarbon base would

provide the greatest stability

5 The influence of the drug on the consistency of the ointment

base

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Routes of skin Penetration
There are two diffusional routes to penetrate intact skin:

The Transappendageal route: 1 2

Include transport via:

1- Hair follicles and sebaceous

glands

2- Sweat glands

➢These routes avoid penetration through the stratum corneum

and therefore known as shunt routes.

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➢ Although these routes offer high permeability, they are of

minor importance because of their relatively small area,

0.1% of the total skin area.

➢The transappendageal route

seems to be most important for ions 1 2

and large polar molecules which

hardly permeate through the

stratum corneum.

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Transepidermal transport means that

molecules cross the intact horny layer

stratum corneum

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Two potential micro-routes are existing

*The transcellular (intracellular) rout

*The intercellular pathways

The principal pathway taken by

drugs is decided by its partition

coefficient

Hydrophilic drugs partition into the intracellular (Transcellular)

pathways, whereas lipophilic drugs traverse the stratum

corneum via the intercellular route.

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Factors Affecting Percutaneous Absorption

Percutaneous absorption is the absorption of substances from

outside the skin to positions beneath the skin, including

entrance into the blood stream.

❑ Factors concerning the nature of the drug

❑ Factors concerning the nature of the vehicle

❑ Factors concerning the condition of the skin

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❑ Factors concerning the nature of the drug

1. Drug concentration Percutaneous absorption

2. Drug partition coefficient (greater attraction to the skin

than to the vehicle) Percutaneous absorption

3. Molecular weight below 800

Percutaneous absorption

4. Particle Size

Percutaneous absorption

5. Solubility in mineral oil and water

Percutaneous absorption

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❑Factors concerning the nature of the vehicle

1. Spreadability of the vehicle

Percutaneous absorption

2. Mixing with the sebum

Percutaneous absorption

3. Hydration of the skin Percutaneous absorption

Oleaginous vehicles act as moisture barriers through which

the sweat from the skin cannot pass, thus increased hydration

of the skin beneath the vehicle and increase Percutaneous

absorption.

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❑ Factors concerning the condition of the skin

Transdermal absorption follow Fick’s First Law of Diffusion

Js = Km D Cs

E

Js = Flux of solute through the skin.

Km = Distribution coefficient of drug between vehicle and

stratum corneum.

D = Membrane Diffusion coefficient for drug in stratum

corneum.

Cs = Concentration difference of solute across the

membrane.

E = Thickness of stratum corneum.

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1. The thickness stratum corneum

Percutaneous absorption

2. Multiple application dosing

Percutaneous absorption than single Application

3. Time of contact with the skin

Percutaneous absorption

4. Broken skin permit (remove of the stratum corneum)

Percutaneous absorption

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Creams are homogeneous, semi-solid preparations consisting of
opaque emulsion systems.
Consistency depends on the type of emulsion whether the cream is
W/O or O/W, and on the nature of the solids in the internal phase.
Creams are intended for the application to the skin or certain
mucous membranes for protective, therapeutic, or prophylactic
purposes, especially where an occlusive effect is not necessary.

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❖are homogeneous, semi-solid preparations containing high
concentrations of insoluble powdered substances (usually not
less than 20%) dispersed in a suitable base.

❖The pastes are usually less greasy, more absorptive, and
stiffer in consistency than ointments because of the large
quantity of powdered ingredients present
❖For example teeth paste

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i. Gels are semi solid system in which liquid phase
is constrained With a 3-d polymeric matrix
having a high degree of physical Or chemical cross
linking by means of gelling agent

ii. Jellies are transparent or translucent non greasy
semisolid and contain more water than gels.

iii. Example of gelling agent; Gelatin, agar, pectin,
tragacanth form gels by this mechanism

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1. (Cataplasma) It is a soft mass of vegetable constituents
or clay, usually heated before application.

2. They are solid or semisolid masses of solid matter
applied to skin in order to Reduce inflammation and in
some cases to act as a counter irritant.

3. After heating the preparation is spread on dressing and
applied to the affected area of the skin.

4. Kaolin poultice BP is prepared by mixing and heating
dried, heavy kaolin and boric acid with glycerin. The
product is spread on a dressing and applied hot to the
skin.

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Plasters are solid or semi solid masses made
by incorporating medicaments in the
resinous or waxy bases which are melted or
spread on suitable baking material..

They are generally used to,

✓Afford protection and medicinal support.

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➢Ingredients used in preparation of semi
solid dosage form:

✓Active pharmaceutical ingredients
✓Bases
✓Preservatives
✓Humectants
✓Anti oxidants
✓Emulsifier
✓Gelling agent
✓Permeation enhancer
✓Buffers

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❖It is one of the most important ingredient used in the
formulation of semisolid dosage form

❖Ointments (oleaginous base, absorption base, water
soluble base, water miscible base)

• Cream (w/o emulsion, o/w emulsion)
• Gel, should contained polymeric matrix
• Plaster- should contain resin (waxy material)

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Some bases , although, resist microbial attack
➢Commonly used preservative include:

Methyl hydroxy benzoate

Benzoic acid

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To prevent hydrolysis of active ingredient.

Example : Butylated hydroxy toluene (BHT)
vitamin _E

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EMULFISIERS:
QUATERNARY AMMONIUM COMPOUNDS (CETRIMIDE)

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Gelling agents
❖ Gelling agent forms a gel dissolves in a liquid phase as a

colloid mixture that forms a weakly cohesive internal
structure.

i. Example of gelling agent; Gelatin, agar, pectin, tragacanth
form gels by this mechanism

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Permeation enhancer
Skin can acts as a barrier with the
introduction of various panetration
enhancers, panetration of the drug through
the skin can be improved. For example –
methanol.

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A humectant is a hygroscopic substance . For
example glycerin

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Buffers are added to variopus purpose such as:

✓ Compatibility with skin

✓ Drug solubility

✓ Drug Stability

✓ Influence on ionization of drug

Example: Sodium acetate , Sodium Citrate

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Methods of
preparation

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PREPARATION OF SEMI SOLIDS

(Ointments, creams, pastes)

Trituration Chemical
method reaction

method
Ex. Ointments Ex. Ointments

creams creams
pastes

Fusion Emulsification
method method

Ex. Ointments Ex. Ointments
creams creams
pastes

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Remington: The Science and Practice of Pharmacy

Pharmaceutics: The Science of Dosage Form Design by Aulton

Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems

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REFRENCES

 

• http://ijpsr.com/bft-article/recent-
advances-in-semisolid-dosage-
form/?view=fulltext

• http://4my5151.blogspot.com/2013/12/c
hapter-6.html?m=1

• https://www.slideshare.net/mobile/rab
abambreen1/semisolid-dosage-form

• https://www.slideshare.net/mobile/doc
mano15/semi-solid-dosage-forms

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